Synthesis and pharmacological activity of substituted imidazolyl- and thiazolylmethylthioethylguanidines
Starting with diphenyl N-benzoyl-carbonimidate impromidine analogues characterized by various substituted imidazole or thiazole groups instead of the 5-methylimidazole part have been synthesized and tested for H2-agonistic and H1-antagonistic activity as well. The most potent substances 6h,i are 20-30 times more active than histamine at the H1-receptors in the isolated spontaneously beating guinea-pig right atrium. In isolated perfused guinea-pig hearts 6h,i were found to predominantly stimulate heart rate, whereas the increase in LVdp/dt(max) was about 40% of impromidine's maximal response.
Buschauer
p. 1003 - 1007
(2007/10/02)
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